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Nimodipine

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Chemical Structure| 66085-59-4 同义名 : BAY-e 9736
CAS号 : 66085-59-4
货号 : A742694
分子式 : C21H26N2O7
纯度 : 95%
分子量 : 418.44
MDL号 : -
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(250.93 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Calcium Channel
描述 L-type calcium (Ca2+) channel mediates influx of calcium ions into the cytoplasm, and thereby triggers calcium release from the sarcoplasm. Calcium channel also plays an important role in excitation-contraction coupling in the heart and is required for normal heart development and normal regulation of heart rhythm. Calcium channel is required for normal contraction of smooth muscle cells in blood vessels and in the intestine. Calcium channel blockers are in clinical use in the fields of diseases such as hypertension, angina. Nimodipine is a L-type calcium channel antagonist. In an experiment utilizing rabbit hippocampal CA1 neurons derived from young or aging rabbits, the time course of calcium action potentials (AP) were tested. Nimodipine decreased the plateau phase of the calcium AP at concentrations as low as 100 nM in aging neurons and 10 μM in young neurons. Switching to higher concentrations of nimodipine did not reveal any substantially increased block of the calcium AP plateau phase[3]. In another report, perilymph spaces of guinea pig cochleae were perfused with artificial perilymph solutions containing 0.1 - 10 μM nimodipine at a rate of 2.5 microliters/min for 10 min. Cochlear perfusion of nimodipine resulted in reversible, dose-related suppression of the compound action potential of the auditory nerve, a prolongation of N1 latency at suprathreshold levels, an elevated CAP threshold, a decrease in N1 latency at a constant amplitude measured at CAP threshold, a reduction in cochlear microphonics, and a reduction of the negative summating potential to a point where it became positive, while the endocochlear potential was not affected[4]. Based on an animal experiment recording nose-poke response to test cocaine and morphine intravenous self-administration in drug-naive mice, a single injection of nimodipine administrated s.c. 80 min prior to the experiment at the doses between 5 – 20 mg/kg inhibited nose-poke response of mice in a dose-related manner. The ED50s of nimodipine against cocaine and morphine self-administration was 14.5 mg/kg and 11.4 mg/kg, respectively[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03434314 Aortic Aneurysm, Thoracoabdomi... 展开 >>nal 收起 << Not Applicable Not yet recruiting September 2021 Austria ... 展开 >> Medizinische Universität Innsbruck Not yet recruiting Innsbruck, Austria Contact: Michael Grimm, Prof. Dr.    +43 512 504 22500    michael.grimm@tirol-kliniken.at    Contact: Johannes Holfeld, Dr.       johannes.holfeld@i-med.ac.at    Herzzentrum Hietzing Not yet recruiting Vienna, Austria Contact: Martin Grabenwöger, Prof. Dr.    +43 1 4020585    Martin.Grabenwoeger@wienkav.at    Contact: Gabriel Weiss, Dr.       gabriel.weiss@wienkav.at    France University Hospital of Bordeaux Not yet recruiting Bordeaux, France Contact: Eric Ducasse, Prof. Dr.    +335 56 79 55 25    eric.ducasse@chu-bordeaux.fr    Marie Lannelongue Hospital Not yet recruiting Le Plessis-Robinson, France Contact: Stephan Haulon, Prof. Dr.          Germany Uniklinik RWTH Aachen Not yet recruiting Aachen, Germany Contact: Michael Jacobs, Prof. Dr.    +49 241 8085197    mjacobs@ukaachen.de    Contact: Drosos Kotelis, Dr.       dkotelis@ukaachen.de    Deutsches Herzzentrum Berlin Not yet recruiting Berlin, Germany Contact: Volkmar Falk, Prof. Dr.       falk@dhzb.de    Contact: Semih Buz, Dr.       buz@dhzb.de    Universitätsklinikum Düsseldorf Not yet recruiting Düsseldorf, Germany Contact: Hubert Schelzig, Prof. Dr.    0049 211 81 07211    hubert.schelzig@med.uni-duesseldorf.de    Contact: Alexander Oberhuber, Dr.       Alexander.Oberhuber@med.uni-duesseldorf.de    Westdeutsches Herz und Gefäßzentrum Essen Not yet recruiting Essen, Germany Contact: Heinz Jakob, Prof. Dr.    +49 201 723 4901    heinz.jakob@uk-essen.de    Contact: Konstantinos Tsagakis, Dr.       Konstantinos.Tsagakis@uk-essen.de    Universitäts-Herzzentrum Freiburg/ Bad Krozingen Not yet recruiting Freiburg, Germany Contact: Martin Czerny, Prof. Dr.    +49 7633 402 6216    martin.czerny@universitaets-herzzentrum.de    Herzzentrum Hamburg Not yet recruiting Hamburg, Germany Contact: Tilo Kölbel, Prof. Dr.    +49 40 7410 58609    t.koelbel@uke.de    Medizinische Hochschule Hannover Not yet recruiting Hanover, Germany Contact: Axel Haverich, Prof. Dr.    0049 511- 532 6580    haverich.axel@mh-hannover.de    Contact: Malakh Shrestha, Prof. Dr.    0049 511- 532 6238    Shrestha.Malakh.lal@mh-hannover.de    Universitätsklinikum Heidelberg Not yet recruiting Heidelberg, Germany Contact: Dittmar Böckler, Prof. Dr.    0049 6221 56 6249    dittmar.boeckler@med.uni-heidelberg.de    Contact: Moritz Bischoff, Dr.       moritz.bischoff@med.uni-heidelberg.de    Herzzentrum Leipzig Not yet recruiting Leipzig, Germany Contact: Christian D Etz, Prof. Dr.    +49 341 865 251007    christian.etz@medizin.uni-leipzig.de    UniversitätskIinikum Leipzig Not yet recruiting Leipzig, Germany Contact: Scheinert Dierk, Prof.Dr.    +49 341 97 18770    dierk.scheinert@medizin.uni-leipzig.de    Klinikum rechts der Isar (TU München) Not yet recruiting Munich, Germany Contact: Hans-Henning Eckstein, Prof. Dr.    +49 89 4140 9244    H.H.Eckstein@lrz.tum.de    Contact: Sarah Geisbüsch, Dr.       sarah.geisbuesch@mri.tum.de    Klinikum der Universität München (LMU) Not yet recruiting München, Germany Contact: Maximilian Luehr, Dr.    + 49 89 4400 72436    maximilian.luehr@med.uni-muenchen.de    St. Franziskus-Hospital GmbH Not yet recruiting Münster, Germany Contact: Giovanni Torsello, Prof. Dr.    0049 251 935-3933    giovanni.torsello@ukmuenster.de    Contact: Theodosios Bisdas, Dr.       theodosios.bisdas@sfh-muenster.de    Paracelsus Universität - Klinikum Nürnberg Not yet recruiting Nuremberg, Germany Contact: Eric Verhoeven, Prof. Dr.    0049 911 398 117004    eric.verhoeven@klinikum-nuernberg.de    Contact: Athanasios Katsargyris, Dr.       Athanasios.Katsargyris@klinikum-nuernberg.de    Universitätsklinikum Regensburg Not yet recruiting Regensburg, Germany Contact: Karin Pfister, Prof. Dr.    +49 941 944 6911    Karin.Pfister@klinik.uni-regensburg.de    Contact: Piotr Kasprzak, Prof. Dr.       piotr.kasprzak@ukr.de    Universitätsklinikum Tübingen Not yet recruiting Tübingen, Germany Contact: Christian Schlensak, Prof. Dr.    0049 7071 29 86638    christian.schlensak@med.uni-tuebingen.de    Contact: Mario Lescan, Dr.       mario.lescan@med.uni-tuebingen.de    Italy S.Orsola-Malpighi Hospital Not yet recruiting Bologna, Italy Contact: Davide Pacini, Prof. Dr.    +39 051 6363329    davide.pacini@unibo.it    Ospedale San Raffaele SRL Not yet recruiting Milano, Italy Contact: Roberto Chiesa, Prof. Dr.    +39 02 2643 7148    chiesa.roberto@unisr.it    Contact: Germano Melissano, Prof. Dr.    +39 02 2643 7148    melissano.germano@hsr.it    Netherlands Maastricht University Medical Center Not yet recruiting Maastricht, Netherlands Contact: Michael Jacobs, Prof. Dr.       m.jacobs@mumc.nl    Contact: Barend Mees, Dr.    +31 43 3877478    barend.mees@mumc.nl    Poland Medical University of Warsaw Not yet recruiting Warsaw, Poland Contact: Tomasz Jakimowicz, Dr.       tomj@wum.edu.pl    Silesian Center for Heart Diseases Not yet recruiting Zabrze, Poland Contact: Marian Zembala, Prof. Dr.    +48 323733689    m.zembala@sccs.pl; sek.kch@sccs.pl    Contact: Maciej K Kolowca, Dr.       maciej@kolowca.eu    Sweden Lund University Hospital Malmoe Not yet recruiting Malmö, Sweden Contact: Tim Resch, Dr.       tim.resch@med.lu.se    Örebro University Hospital Not yet recruiting Örebro, Sweden Contact: Thomas Larzon, Prof. Dr.       thomas.larzon@regionorebrolan.se    Switzerland Bern University Hospital Not yet recruiting Bern, Switzerland Contact: Jürg Schmidli, Prof. Dr.    +41 31 632 26 02    juerg.schmidli@insel.ch    United Kingdom St Bartholomews Hospital Not yet recruiting London, United Kingdom Contact: Aung Y Oo, Prof. Dr.       AungYe.OO@Bartshealth.nhs.uk 收起 <<
NCT03718780 Pulmonary Disease, Chronic Obs... 展开 >>tructive Lung Diseases, Interstitial Chronic Heart Failure Pulmonary Arterial Hypertension Hyperventilation Syndrome Healthy 收起 << Not Applicable Not yet recruiting March 2020 France ... 展开 >> Service de pneumologie Not yet recruiting Béthune, France, 62408 Contact: Frédéric BART          Principal Investigator: Frédéric BART          Service de pneumologie CHMS Not yet recruiting Chambéry, France, 73000 Contact: Serge Kouzan          Sub-Investigator: Julien PERNOT          Sub-Investigator: Marie COUDURIER          Principal Investigator: Serge KOUZAN          Service de réanimation médicale - CHMS Not yet recruiting Chambéry, France, 73000 Contact: Jean-Marc THOURET       Jean-Marc.Thouret@ch-metropole-savoie.fr    Contact: Vincent PEIGNE       vincent.peigne@ch-metropole-savoie.fr    Sub-Investigator: Jean-Marc THOURET          Principal Investigator: Vincent PEIGNE          Service de Pneumologie CHU Grenoble Not yet recruiting La Tronche, France, 38700 Contact: Bernard AGUILANIU          Principal Investigator: Bernard AGUILANIU 收起 <<
NCT00001478 - Completed - United States, Maryland ... 展开 >> National Institute of Mental Health (NIMH) Bethesda, Maryland, United States, 20892 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.39mL

0.48mL

0.24mL

11.95mL

2.39mL

1.19mL

23.90mL

4.78mL

2.39mL
参考文献

[1]Bork K, Wurm F, et al. Neuroprotective and neuroregenerative effects of nimodipine in a model system of neuronal differentiation and neurite outgrowth. Molecules. 2015 Jan 9;20(1):1003-13.

[2]Koskimaki J, Matsui N, et al. Nimodipine activates TrkB neurotrophin receptors and induces neuroplastic and neuroprotective signaling events in the mouse hippocampus and prefrontal cortex. Cell Mol Neurobiol. 2015 Mar;35(2):189-96.

[3]Moyer JR Jr, Disterhoft JF. Nimodipine decreases calcium action potentials in rabbit hippocampal CA1 neurons in an age-dependent and concentration-dependent manner. Hippocampus. 1994 Feb;4(1):11-7.

[4]Bobbin RP, Jastreboff PJ, Fallon M, Littman T. Nimodipine, an L-channel Ca2+ antagonist, reverses the negative summating potential recorded from the guinea pig cochlea. Hear Res. 1990 Jul;46(3):277-87.

[5]Kuzmin A, Zvartau E, Gessa GL, Martellotta MC, Fratta W. Calcium antagonists isradipine and nimodipine suppress cocaine and morphine intravenous self-administration in drug-naive mice. Pharmacol Biochem Behav. 1992 Mar;41(3):497-500.